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AICAR (5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside, 5-aminoimidazole-4-carboxamide ribonucleoside, acadesine) is each of several interesting things. First, it’s an important pharmacological research agent, used principally as an AMPK activator. It’s a compound which has shown extremely impressive fat-loss and endurance-enhancing effects in laboratory animals. Further, it has considerable mystique resulting from at least some use by elite European cyclists. And lastly, it’s readily available from research chemical sites and is being personally tried by many, though generally as part of stacks and combined with changes in training and/or diet.
AICAR’s principal mechanism of action is activation of AMPK (AMP-activated protein kinase.) As is well known, ATP (adenosine triphosphate) is produced by mitochondria as a ready-to-use energy source for biochemical processes in the cell. These processes do not use glucose, fats, or fatty acids directly as energy sources: these must first be metabolized in the mitochondria to yield ATP. When ATP is used for energy, its first product is ADP (adenosine di-phosphate), and then – if the cell is really deprived of immediate sources of energy – finally to AMP (adenosine monophosphate.)
AMP only accumulates as a cell becomes energy-deprived. Accordingly, there’s a system where the cell detects any low energy state from the concentration of AMP that’s present, and activates AMPK in response.
AMPK in turn ramps up conversion of fuel sources, including fatty acids, into ATP, as well as stimulating quite a number of other systems in the cell.
Activating AMPK, therefore, causes the same cellular machinery (so to speak) to be turned on as if the cell were energy deprived, for example from intensive exercise, or from low caloric intake.
AICAR, at sufficient and quite substantial concentration, is effective at activating AMPK and inducing a cellular state as if exercise had been performed, or energy stores were low and fat therefore needed to be burned.
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